氨基哌啶类化合物的设计合成及其对单胺递质再摄取的抑制活性.pdfVIP

20 6 Vol20 No6 p. 476 2010 12 98 Ch inese Journal of M ed i inalC hem istry De 2010 Sum 98 : 1005- 0108( 20 10) 06- 0476- 08 4 1 2 2 1* 郑永勇 , 俞蕾平, 郭琳 , 李建其 ( 1. , 200040; 2. , 20 1203) : 4 ( 5HT /NA /DA) 4N , ! 1 ~ ! 9, ! 10 ~ ! 17 ; , 17, 5 : 4; ; : R914 : A Design, synthesis and m onoam ine reuptake inhibitors activities of 4am inop iperidine derivatives 1 2 2 1* ZHENG Y ongyong , YU L eip ing , GUO L in , L I Jianqi ( 1. Shanghai Institute of Pharma eu ti al Industry, Shanghai 200040, Ch ina; 2. Shanghai Institute ofM ateria M edi a, Chinese A adem y of S ien es, Shanghai 201203, Ch ina ) Abstract: A im To design and synthesize 4am inopiperid ine derivatives m onoam ine reuptake inhibitors. M ethods The target om pounds ! 1 - ! 9 w ere prepared by N alkylation of 4am inop iperid ine derivatives, and om pounds ! - ! w ere obtained by redu tion of ompounds ! - ! w ith N aBH . R esu ts and 10 17 1 9 4 con c u sion Seventeen new target ompounds w ere synthesized and their stru tures w ere onfirmed by HR 1 M S and HNM R. The resu lts of prelmi inary pharm a ologi al test show ed that five of seventeen om pounds possessed d iversem onoam ine reuptake inhibitors a tivities. K ey w ord s: 4am inop iperid ine; monoam ine reuptake inhibitor; syn thesis , 2~ 3 [ 2] (M AO Is) ( TCA s), , 5 , HT /NA (